Bombesin (7-14) derivative: Radiochemical evaluation using different spacers

International Conference on Nuclear Chemistry

December 08-09, 2016 San Antonio, USA

Nourollah Sadeghzadeh, Hadi Pisshsaraie, Yaser Ghasemi and Iman Emrarian

Mazandaran University of Medical Sciences, Iran

Posters & Accepted Abstracts: J Nucl Med Radiat Ther

Abstract :

Several strategies have been used in the design and development of diagnostic radiopharmaceuticals for early detection of human cancer. The spacer technology seems to be one of the most promising approaches concerning the design of new Bombesin analogues since spacer would be to prevent possible interaction between the radiometal-chelator complex and the receptor binding region of the biomolecule, which has influence on tumor /normal organ ration. The spacer can also act as a pharmacokinetic modifier. Moreover the spacers effect on the function of 99mTc-labeled peptide- HYNIC conjugate and their ability. The aim of this study was to evaluate the radiochemical and to determine the effects on ability of bombesin derivative labeled with 99mTc via hydrazinonicotinamide (HYNIC) with tripeptidic (Ser- Ser - Ser) and (Gly-Gly-Gly) spacer. Prepared bombein- HYNIC conjugates radio-labeled with 99mTc using tricine and ethylenediamine diacetic acid (EDDA) as exchange labeling method at 100�°C for 10 min and radiochemical analysis involved ITLC and HPLC methods. The stability of radiopeptide was checked in the presence of human serum at 37�°C and saline up to 24 h. [99mTc-EDDA/tricin/HYNIC-(Ser)3- D-Phe13]BN(7-14) and [99mTc-EDDA/tricin/HYNIC-(Gly)3-D-Phe13]BN (7-14) were obtained with Radiochemical purities of >95%. Results of in-vitro studies demonstrated a high stability in serum and saline. Radio-labeling of this novel conjugates with 99mTc easily were performed using exchange labeling and high radiochemical yields achieved. The prepared99mTc-HYNICBombesin conjugates demonstrated some potential as site-directed diagnostic radiopharmaceuticals; therefore, in vivo studies are required and are being carried out.

Biography :

Email: nourollahsadeghzadeh@yahoo.com